Incorporation of Stable Pseudopeptide Bonds: Methylene Amino, Thioether, and Hydroxyethylene Derivatives
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The introduction of pseudopeptide bonds (amide bond surrogates) into the peptide backbone during synthesis is now a common
technique in peptide chemistry (1
). These pseudo-peptide bonds are introduced in order to satisfy criteria such as stability to enzymatic degradation, transition
state analogs/enzyme inhibition, alteration in peptide backbone conformation (with corresponding changes in flexibility and
hydrogen-bonding character), increased receptor specificity, increased potency, and biological responses (2
).
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